Membrane Transporters-Ion Channels

Items 251-300 of 2532

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  1. (-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca2+-permeable nonselective cation channel, to increase [Ca2+]i. Antitumor activity.
  2. 5-HT3 receptor inhibitor

    Eucalyptol is a bicyclic monoterpene that has been found in Eucalyptus and other plants. It is an inhibitor of 5-HT3 receptor ,potassium channel, TNF-α and IL-1β.
  3. TRPV1 antagonist

    Mavatrep is an orally bioavailable TRPV1 antagonist (Ki=6.5 nM), exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6.
  4. MCT inhibitor

    7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in cancer cells.
  5. MCT Inhibitor?€?

    7ACC1 selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.
  6. TRPM8 antagonist

    RQ-00203078 is a highly selective, potent and orally available TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively), exhibits >350-fold selectivity for TRPM8 over TRPV4, TRPV1 and TRPA1.
  7. F508del-CFTR trafficking corrector

    KM 11060 corrects F508del-CFTR trafficking, increasing the amount of functional CFTR at the plasma membrane (~75%) and Inhibits PDE5 activity
  8. TRPV4 Activator

    GSK1016790A is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34nM in choroid plexus epithelial cells.
  9. TRPV1 receptor antagonist

    SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist.
  10. Ferroptosis inhibitor

    RSL3 is a ferroptosis activator in a VDAC-independent manner,exhibiting selectivity for tumor cells bearing oncogenic RAS.
  11. Calcium Channel Activator

    Bay K 8644 is a potent, selective activator of L-type Ca2+ channel with IC50 of 17.3 nM.
  12. hERG channel activator

    NS-1643 is a Human ether-a-go-go related gene (hERG) KV11.1 channel activator (EC50 = 10.5 uM).
  13. Oct4 activator

    OAC2 is an Oct4-activating compound which activates expression through the Oct4 gene promoter.
  14. Doxapram inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively. Doxapram is a respiratory stimulant. Administered intravenously, doxapram stimulates an increase in tidal volume, and respiratory rate.
  15. SUR/URAT1 inhibitor

    Lesinurad is a selective uric acid re-absorption inhibitor (SURI) and is also a selective inhibitor of URAT1, a transporter in the kidney that regulates uric acid excretion from the body.
  16. Potassium channel activator

    NS1619 is a Bkca opener or large-conductance Ca2+-activated potassium (BKCa, KCa1.1) channel activator.
  17. sodium channel inhibitor

    Levobupivacaine is a local anaesthetic drug belonging to the amino amide group.
  18. p97 ATPase inhibitor

    ML241 is a potent and selective inhibitors of p97 ATPase. ML241 inhibit p97 ATPase with IC(50) values of 100 nM.
  19. HIV integrase inhibitor

    GSK744 is a potent HIV integrase inhibitor as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection.
  20. P-gp inhibitor

    MC-70 is a potent P-gp inhibitor (EC50 = 0.69 uM).
  21. Oct3/4 inducer

    O4I2 is a potent inducers of Oct3/4. O4I2 showed high activity in enforcing Oct3/4 expression. O4I2 is a new class of small molecules suitable for iPSC generation.
  22. MSCs Inhibitor

    GsMTX4 is a 34 amino acid peptidyl toxin isolated from the Grammostola rosea (Chilean rose) tarantula venom and belongs to the huwentoxin-1 family.
  23. AMPA/kainate antagonist

    CNQX is a competitive, non-NMDA glutamate receptor antagonist (IC50s = 0.3 and 1.5 uM for AMPA and kainate receptors, respectively, versus IC50 = 25 uM for NMDA receptors).
  24. AMPA/kainate antagonist

    CNQX disodium salt, water-soluble form of AMPA/kainate antagonist CNQX (GLXC-11053).
  25. Benzocaine hydrochloride is a surface anesthetic that acts by preventing transmission of impulses along nerve fibers and at nerve endings.
  26. voltage-gated sodium channel inhibitor

    Procaine is a benzoic acid derivative with local anesthetic and antiarrhythmic properties.
  27. Dantrolene sodium Hemiheptahydrate is a skeletal muscle relaxant that acts by interfering with excitation-contraction coupling in the muscle fiber.
  28. proton pump inhibitor

    Rabeprazole sodium is an antiulcer drug in the class of proton pump inhibitors.
  29. CaCC activator

    Eact activates the Calcium-activated Chloride channel (CaCC) TMEM16A CaCC.
  30. K+ Channel inhibitor

    K+ Channel inhibitor, building block for synthesis of dihydropyrazolopyrimidine inhibitors of Kv1.5 (IKur).
  31. URAT1 inhibitor

    UR 1102, inhibitor of the renal urate transporter URAT1 with high selectivity to URAT1 over OAT1 and OAT3 in vitro (Ki values 0.057 uM, 7.2 uM, and 2.4 uM, respectively), capable of increasing the fractional excretion of urinary uric acid, and reducing plasma uric acid more effectively than Benzbromarone.
  32. BCRP inhibitor

    KS-176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter (IC50 values are 0.59 and 1.39 uM in Pheo A and Hoechst 33342 assays respectively).
  33. VMAT2 inhibitor

    Valbenazine is a potent and selective VMAT2 inhibitor.
  34. Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity.
  35. Wnt/beta-catenin inhibitor

    Hexachlorophene is a potent KCNQ1/KCNE1 potassium channel activator with EC50 of 4.61 ?? 1.29 uM; also is an inhibitor of Wnt/beta-catenin signaling.
  36. SINE/CRM1 inhibitor

    KPT276, analog of KPT-185, is a selective inhibitor of nuclear export (SINE) and CRM1.
  37. CRAC channel inhibitor

    YM-58483 is the first selective and potent inhibitor of CRAC channels and subsequent Ca2+ signals.
  38. Proton pump inhibitor

    Lauric acid is a proton pump inhibitor potentially for the treatment of helicobacter pylori infections.
  39. Sodium Channel Blocker

    Pilsicainide is a water soluble selective Na+ channel blocker.
  40. Nav1.7 Inhibitor

    PF-05089771 is a Selective Nav1.7 Inhibitor (IC50 = 11 nM) that interacts with the voltage-sensor domain (VSD) of domain IV.
  41. Sodium Channel inhibitor

    AmbroxolHCl is a potent inhibitor of the neuronal Na+ channels, inhibits TTX-resistant Na+ currents with IC50 of 35.2 uM and 22.5 μM for tonic and phasic block, inhibits TTX-sensitive Na+ currents with IC50 of 100 μM. Phase 3.
  42. Amoxapine is a tricyclic dibenzoxazepine (an N-aryl piperazine) which acts similarly to several other tricyclic antidepressants, amoxapine inhibits GLYT2a transport activity with IC50 of 92 μM.
  43. Camphor is a waxy, flammable, white or transparent solid with a strong aroma, often used to relieve pain, reduce itching and treat fungal infections. It can activate TRPV1 and TRPV3
  44. Chlorocresol is an activator of ryanodine receptor.
  45. Chlorpropamide is a sulfonylurea class drug for type 2 diabetes mellitus.
  46. Cinepazide maleate is a maleate salt form of cinepazide which is a vasodilator.
  47. calcium channel blocker

    Cinnarizine is a medication derivative of piperazine, and characterized as an antihistamine and a calcium channel blocker.
  48. proton pump inhibitor

    (R)-Lansoprazole is a proton pump inhibitor which prevents the stomach from producing acid.
  49. excitatory transmitter/agonist

    L-Glutamic acid monosodium salt acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). (S)-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
  50. Calcium Channel /TRP5 antagonist

    Lomerizine dihydrochloride is a antagonist at L-type and T-type Ca 2+ channels and TRp5 channels used to treat migraines and vertigo.

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